ArticleActa pharmacologica Sinica2021
DCZ5248, a novel dual inhibitor of Hsp90 and autophagy, exerts antitumor activity against colon cancer.
Article in Acta pharmacologica Sinica, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 11 papers, 1 of them a synthesis that pooled it.
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Who cites it
11 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.
- Antitumor Activity of s-Triazine Derivatives: A Systematic Review.Molecules (Basel, Switzerland) · 2023Pooled it
- RCC1 Domain-Containing Protein 1 Promotes Colon Cancer Malignant Progression by Activating Autophagy-Dependent WNT5A Secretion in Cancer-Associated Fibroblasts.Journal of the Royal Society of New Zealand · 2026Article
- Interaction mechanisms between autophagy and ferroptosis: Potential role in colorectal cancer.World journal of gastrointestinal oncology · 2023Review
- Nitidine chloride induces cardiac hypertrophy in mice by targeting autophagy-related 4B cysteine peptidase.Acta pharmacologica Sinica · 2023Article
- Evaluation of the Heat Shock Protein 90 Inhibitor Ganetespib as a Sensitizer to Hyperthermia-Based Cancer Treatments.Cancers · 2022Article
- Heterocyclic Compounds as Hsp90 Inhibitors: A Perspective on Anticancer Applications.Pharmaceutics · 2022Review
- Regulated cell death (RCD) in cancer: key pathways and targeted therapies.Signal transduction and targeted therapy · 2022Review
- Cinnamomi Ramulus inhibits the growth of colon cancer cells via Akt/ERK signaling pathways.Chinese medicine · 2022Article
- Inhibiting Cytoprotective Autophagy in Cancer Therapy: An Update on Pharmacological Small-Molecule Compounds.Frontiers in pharmacology · 2022Review
- Autophagy inhibition and microRNA‑199a‑5p upregulation in paclitaxel‑resistant A549/T lung cancer cells.Oncology reports · 2021Article
- Autophagy Modulators in Cancer Therapy.International journal of molecular sciences · 2021Review
Corrections and comments
- Erratum issued
Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Hsp90 is a potential therapeutic target for tumor, as it maintains the stability of a variety of proteins related to tumor development and progression. Autophagy is a self-degradation process to maintain cellular homeostasis and autophagy inhibitors can suppress tumor growth. In this study, we identified DCZ5248, a triazine derivative, was a dual inhibitor of both Hsp90 and late-autophagy with potent antitumor activity against colon cancer cells in vitro and in vivo. We showed that DCZ5248 (0.1-10 μM) induced dose-dependent degradation of Hsp90 client proteins (AKT, CDK4, CDK6 and RAF-1) in HCT 116 colon cancer cells through a proteasome-dependent pathway. Meanwhile, DCZ5248 (0.3 μM) induced cytoplasmic vacuole formation, LC3 II conversion, p62 protein upregulation, and inhibited autophagy at the late stage in the colon cancer cell lines tested. We further revealed that the inhibition of autophagy was achieved by impairing lysosomal functions through induction of lysosomal acidification and attenuation of lysosomal cathepsin activity. The modulation of autophagy by DCZ5248 was independent of Hsp90 inhibition as the autophagy inhibition was not blocked by Hsp90 knockdown. Importantly, inhibition of both Hsp90 function and autophagy by DCZ5248 induced G
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